TD-198946-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETD-198946Cat. No.: HY-15642CAS No.: 364762-86-7分式: CHNOS分量: 482.55作靶點(diǎn): Others作通路: Others儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 28 mg/mL (58.03 mM)* means soluble, but saturation un

2、known.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.0723 mL 10.3616 mL 20.7232 mL5 mM 0.4145 mL 2.0723 mL 4.1446 mL10 mM 0.2072 mL 1.0362 mL 2.0723 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 TD-198946種噻吩并唑衍物。它 種效的軟形成劑。體外研究TD-198946 is a potent chondrogenic agent. TD-

3、198946 strongly induces chondrogenic differentiation withoutpromoting hypertrophy in cell and metatarsal organ cultures. TD-198946 induces stronger Col2a1 promoteractivity than insulin in ATDC5 cells. In C3H10T1/2 cells, ATDC5 cells and primary mouse chondrocytes, TD-198946 dose-dependently stimulat

4、es endogenous expression of the chondrocyte markers Col2a1 and Acan,1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEwith maximum effects around 1-10 M 1.體內(nèi)研究 When administered directly into the joint space, TD-198946 successfully prevents and repaires degenerationof the articular cartilage. TD-1989

5、46 exerts its effect through the regulation of Runx1 expression, which isdownregulated in both mouse and human OA cartilage compared with normal tissue 1. TD-198946 hasdisease-modifying effects on progressed osteoarthritis. TD-198946 may prevent the progression ofosteoarthritis by acting on the rema

6、ining chondrocytes rather than repairing damaged cartilage, it may bemost effective as a therapeutic during the early or middle stages of osteoarthritis, before the articularcartilage is fully eroded 2. Cartilaginous cell-sheets are generated by culturing mouse and canine costalchondrocytes and huma

7、n mesenchymal stem cells with TD-198946 on temperature-responsive dishes. Thetransplanted cell-sheets are then successfully used to promote the reconstruction of permanent cartilage,with no evidence of chondrocyte hypertrophy in the knee articular cartilage defects created in mice andcanines 3.PROTO

8、COLAnimal Mice: Each of the prevention and repair models had two groups: (1) TD-198946-treated animals and (2)Administration 1 saline-treated animals. In all the mice tested the left knee joints underwent the operation and the right kneejoints are sham-operated. Mice are re-anaesthetised and given a

9、 10 L intra-articular injection of TD-198946or saline immediately after surgery (prevention model) or 4 weeks following surgery (repair model) every 5days for 8 or 4 weeks, respectively 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Yano

10、 F, et al. A novel disease-modifying osteoarthritis drug candidate targeting Runx1. Ann Rheum Dis. 2013 May;72(5):748-53.2. Yano F, et al. Disease-modifying effects of TD-198946 on progressed osteoarthritis in a mouse model. Ann Rheum Dis. 2014Nov;73(11):2062-4.3. Yano F, et al. Cell-sheet technology combined with a thienoindazole derivative small compound TD-198946 for cartilage regeneration.Biomaterials. 2013 Jul;34(22):5581-7.McePdfHeightCaution: Product has not been ful